Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 102, Issue -, Pages 334-351Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2015.08.003
Keywords
Pyrazolo[3,4-h]quinolines; Photodynamic therapy; Antiproliferative activity; Photosensitizing agents; Reactive oxygen species; PUVA therapy
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Funding
- Ministero dell'Istruzione dell'Universita e della Ricerca
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A new series of pyrazolo[3,4-h]quinolines, heteroanalogues of angelicin was conveniently prepared with a broad substitution pattern. A large number of derivatives was obtained and the cellular photocytotoxicity was evaluated in vitro against 5 different human tumor cell lines with GI(50) values reaching the nanomolar level (14.52-0.04 mu M). Selected compounds were able to photoinduce a massive cell death with the involvement of mitochondria. Their photodamage cellular targets were proteins and lipids and they did not cause any kind of DNA photodamage. This latter event is of considerable importance in the modulation of long term side effects, generally associated with the use of classical furocoumarins. (C) 2015 Elsevier Masson SAS. All rights reserved.
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